MSK

Question 1

Aspirin

• mech, clin use, toxicity
• chronic use ->?
• stim’s?

Answer 1

• irreversibly inhib’s COX1/2 by acetylation -> decr’d syn of TXA2 and PGE/PGI
• low dose to decr plt aggregation, interm dose for antipyretic/analgesic, high dose for anti-inflamm
• gastric ulcers, tinnitus (CNVIII); Reye’s
• ARF, interstitial nephritis, upper GI bl
• resp center -> hypervent and resp alk

Question 2

NSAIDS

• Ex’s
• mech, clin use, tox

Answer 2

• ibuprofen, naproxen, indomethacin, ketorolac, diclofenac
• reversibly inhib COX1/2
• antipyretic, analgesic, anti-inflamm; indomethacin to close PDA
• interstitial nephritis, gastric ulcer, renal ischemia

Question 3

COX-2 inhib’s = ?

- mech, clin use, tox

Answer 3

• Celecoxib
• reversibly inhib COX-2 (found in inflamm cells and vasc endo, mediates inflamm and pain) (spares GI and TXA2 plt func)
• RA, OA, use in pt’s w/ gastritis/ulcers
• incr’d risk of thrombosis, sulfa allergy

Question 4

Acetaminophen

• mech, clin use, tox
• overdose antidote

Answer 4

• reversibly inhib’s cyclooxygenase, mostly in CNS
• antipyretic, analgesic, NOT anti-inflamm, use instead of aspirin for no Reye’s in kids w/ viral infec
• overdose -> hep necrosis; metab depletes glutathione and toxic to liver
• N-acetylcysteine - regen’s glutathione

Question 5

Bisphosphonates

• Ex’s
• mech, clin use, tox

Answer 5

• Alendroate and other -dronates
• pyrophosphate analogues, bind hydroxyapatite in bone -> inhib’s osteocl’s
• osteoporosis, hyperCa, Paget’s dz of bone
• corrosive esophagitis, osteonecrosis of jaw

Question 6

• Treat gout w/? (overproducer vs. underexcretor)

- Acute gout drugs?

Answer 6

• Overproducer: allopurinol, febuxostat
  Underexcretor: probenecid, cochicine
• NSAIDs, gcc’s

Question 7

Allopurinol

• mech
• used in
• see incr’d conc’s of
• don’t give w/

Answer 7

• inhib’s xanthine oxidase -> less uric acid made
• gout, prevent tumor lysis synd
• azathioprine and 6-MP bc also metab’d by X.O.
• salicylates bc depress uric acid clearance

Question 8

Febuxostate

• mech
• use for

Answer 8

• inhib’s xanthine oxidase

- gout

Question 9

Probenecid

• mech
• use for

Answer 9

• inhib’s resorb of uric acid in PCT (also inhib’s Pn secretion)
• gout

Question 10

Cochicine

• mech
• use for
• SEs

Answer 10

• binds and stabilized tubulin to inhib polymerization -> no leukocyte chemotaxis and degranulation
• gout
• GI, esp if PO

Question 11

Etanercept

• mech
• use for

Answer 11

• fusion pr from rDNA that is TNF decoy R

- RA, psoriasis, AS

Question 12

Infliximab, adalimumab

• mech
• use for
• SE

Answer 12

• anti-TNF-a mAb
• Crohn’s dz, RA, AS, psoriasis
• predispose to TB since no TNFa -> no act’n of Mphage and thus no destruc of phagocytosed microbes